menu
    • menu

    List of Suppliers' Taste Masking Excipients Application used in 03KSI6WLXH on PharmaCompass.com

    Client Email Product
    ChemWerth works in generic API development & supply, non-infringement patent strategy development and regulatory support.

    Virtual Booth

    Contact Supplier

    FAMAR CDMO- From early development to commercial manufacturing.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-09-09

    Virtual Booth

    Contact Supplier

    Seqens is an integrated global leader in pharmaceutical solutions & specialty ingredients & provides custom-made solutions.

    Access Virtual Booth

    Contact Supplier

    Veranova: A CDMO that manages complexity with confidence.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-09-09

    Virtual Booth

    Contact Supplier

    ACTIVE PHARMA INGREDIENTS

    FINISHED DOSAGE FORMULATIONS

    RELATED EXCIPIENT COMPANIES

    EXCIPIENTS BY APPLICATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    MARKET PLACE

    PharmaCompass

    Synopsis

    Product SearchProduct Search

    Synopsis

    ACTIVE PHARMA INGREDIENTS

    1

    API Suppliers

    API Suppliers

    0

    USDMF

    US DMFs Filed

    0

    CEP/COS

    CEP/COS Certifications

    0

    JDMF

    JDMFs Filed

    0

    EU WC

    EU WC

    0

    KDMF

    KDMF

    0

    NDC API

    NDC API

    0

    VMF

    NDC API

    1

    Listed Suppliers

    Other Suppliers

    API REF. PRICE (USD/KG)

    $
    $ 0

    MARKET PLACE

    3

    API

    0

    FDF

    0INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    2

    FDF Dossiers

    FDF Dossiers

    0

    FDA Orange Book

    FDA (Orange Book)

    2

    Europe

    Europe

    0

    Canada

    Canada

    0

    Australia

    Australia

    0

    South Africa

    South Africa

    0

    Listed Dossiers

    Listed Dossiers

    0 DRUGS IN DEVELOPMENT

    FDF Dossiers

    DRUG PRODUCT COMPOSITIONS

    REF. STANDARDS OR IMPURITIES

    0

    EDQM

    0

    USP

    0

    JP

    0

    Others

    PATENTS & EXCLUSIVITIES

    0

    US Patents

    0

    US Exclusivities

    0

    Health Canada Patents

    DIGITAL CONTENT

    1

    Data Compilation #PharmaFlow

    0

    Stock Recap #PipelineProspector

    0

    Weekly News Recap #Phispers

    11

    News #PharmaBuzz

    GLOBAL SALES INFORMATION

    US Medicaid

    12,094,634

    Annual Reports

    116

    Finished Drug Prices

    Listed Dossiers

    107 RELATED EXCIPIENT COMPANIES

    183EXCIPIENTS BY APPLICATIONS

    Chemistry

    Click the arrow to open the dropdown
    read-moreClick the button for full data set
    read-moreClick the button for full data set
    Also known as: 916072-89-4, S-297995, 03ksi6wlxh, S 297995, S-297,995, (4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-n-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide
    Molecular Formula
    C32H34N4O6
    Molecular Weight
    570.6  g/mol
    InChI Key
    AXQACEQYCPKDMV-RZAWKFBISA-N
    FDA UNII
    03KSI6WLXH
    Naldemedine
    Naldemedine is an opioid receptor antagonist. It is a modified form of [DB00704] to which a side chain has been added to increase molecular weight and polar surface area resulting in restricted transport across the blood brain barrier. Naldemedine was approved in 2017 in both the US and Japan for the treatment of Opioid-induced Constipation.
    Naldemedine is an Opioid Antagonist. The mechanism of action of naldemedine is as an Opioid Antagonist.
    1 2D Structure

    Naldemedine

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-N-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide
    2.1.2 InChI
    InChI=1S/C32H34N4O6/c1-30(2,29-33-27(35-42-29)18-6-4-3-5-7-18)34-28(39)20-15-32(40)22-14-19-10-11-21(37)25-23(19)31(32,26(41-25)24(20)38)12-13-36(22)16-17-8-9-17/h3-7,10-11,17,22,26,37-38,40H,8-9,12-16H2,1-2H3,(H,34,39)/t22-,26+,31+,32-/m1/s1
    2.1.3 InChI Key
    AXQACEQYCPKDMV-RZAWKFBISA-N
    2.1.4 Canonical SMILES
    CC(C)(C1=NC(=NO1)C2=CC=CC=C2)NC(=O)C3=C(C4C56CCN(C(C5(C3)O)CC7=C6C(=C(C=C7)O)O4)CC8CC8)O
    2.1.5 Isomeric SMILES
    CC(C)(C1=NC(=NO1)C2=CC=CC=C2)NC(=O)C3=C([C@H]4[C@@]56CCN([C@@H]([C@@]5(C3)O)CC7=C6C(=C(C=C7)O)O4)CC8CC8)O
    2.2 Other Identifiers
    2.2.1 UNII
    03KSI6WLXH
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    2. S-297995

    3. Symproic

    2.3.2 Depositor-Supplied Synonyms

    1. 916072-89-4

    2. S-297995

    3. 03ksi6wlxh

    4. S 297995

    5. S-297,995

    6. (4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-n-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide

    7. Naldemedine [usan]

    8. Unii-03ksi6wlxh

    9. Naldemedine [usan:inn]

    10. Naldemedine [mi]

    11. Naldemedine [inn]

    12. Naldemedine (usan/inn)

    13. Naldemedine [who-dd]

    14. Gtpl9150

    15. Schembl9880572

    16. Chembl2105755

    17. Dtxsid501030350

    18. Bdbm50503604

    19. Db11691

    20. Compound 9k [pmid: 30446313]

    21. Hy-19627

    22. Morphinan-7-carboxamide, 17-(cyclopropylmethyl)-6,7-didehydro-4,5-epoxy-3,6,14- Trihydroxy-n-(1-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl)-,(5alpha)-

    23. Cs-0016072

    24. J3.573.009e

    25. D10188

    26. Q6960846

    27. 17-(cyclopropylmethyl)-6,7-didehydro-4,5a-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    28. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    2.4 Create Date
    2011-12-27
    3 Chemical and Physical Properties
    Molecular Weight 570.6 g/mol
    Molecular Formula C32H34N4O6
    XLogP33.2
    Hydrogen Bond Donor Count4
    Hydrogen Bond Acceptor Count9
    Rotatable Bond Count6
    Exact Mass570.24783482 g/mol
    Monoisotopic Mass570.24783482 g/mol
    Topological Polar Surface Area141 Ų
    Heavy Atom Count42
    Formal Charge0
    Complexity1140
    Isotope Atom Count0
    Defined Atom Stereocenter Count4
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 1  
    Drug NameSYMPROIC
    Active IngredientNALDEMEDINE TOSYLATE
    CompanySHIONOGI INC (Application Number: N208854. Patents: 9108975, RE46365, RE46375)

    4.2 Drug Indication

    For the treatment of opioid-induced constipation.

    FDA Label

    Rizmoic is indicated for the treatment of opioid-induced constipation (OIC) in adult patients who have previously been treated with a laxative.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Naldemedine is an opioid receptor antagonist with restricted movement across the blood brain barrier. This allows it to antagonize the periperal effects of opioid drugs such as constipation without interfering with the effects on the central nervous system.

    5.2 FDA Pharmacological Classification
    5.2.1 Active Moiety
    NALDEMEDINE
    5.2.2 FDA UNII
    03KSI6WLXH
    5.2.3 Pharmacological Classes
    Opioid Antagonists [MoA]; Opioid Antagonist [EPC]
    5.3 ATC Code

    A06AH05

    A - Alimentary tract and metabolism

    A06 - Drugs for constipation

    A06A - Drugs for constipation

    A06AH - Peripheral opioid receptor antagonists

    A06AH05 - Naldemedine

    5.4 Absorption, Distribution and Excretion

    Absorption

    Tmax is 0.75 h. Administration with a high-fat meal reduces Cmax by 35% and increases Tmax to 2.5 h.

    Route of Elimination

    57% of naldemedine is excreted in the urine with 16-18% as the parent compound and 35% is excreted in the feces.

    Volume of Distribution

    The apparent volume of disribution during the terminal phase is 155 L

    5.5 Metabolism/Metabolites

    Naldemedine is mainly metabolized to nor-naldemedine by CYP3A. Some metabolism to naldemedine-3-glucuronide occurs via UGT1A3. Both metabolites are acitive but less potent than naldemedine. The relative exposures of these metabolites are 9-13% and <3% for nor-naldemedine and naldemedine-3-glucuronide respectively. Naldemedine is also cleaved in the intestine to form benzamidine and naldemedine carboxylic acid.

    5.6 Biological Half-Life

    The terminal elimination half life is 11 h.

    5.7 Mechanism of Action

    Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors. The binding of opioid agonists to peripheral mu-opioid receptors slows the transit of feces through the intestine resulting in constipation. By antagonizing mu-opioid receptors, naldemedine inhibits this effect.

    Related Excipient Companies

    Upload your portfolio for free, ask us

    Excipients by Applications

    Click here to find the perfect excipient manufacturers by their capabilities

    Coating Systems & Additives

    read-more
    read-more

    Fillers, Diluents & Binders

    read-more
    read-more

    Controlled & Modified Release

    read-more
    read-more

    Disintegrants & Superdisintegrants

    read-more
    read-more

    Direct Compression

    read-more
    read-more

    Chewable & Orodispersible Aids

    read-more
    read-more

    Taste Masking

    read-more
    read-more

    Lubricants & Glidants

    read-more
    read-more

    Granulation

    read-more
    read-more

    Film Formers & Plasticizers

    read-more
    read-more

    Empty Capsules

    read-more
    read-more

    Parenteral

    read-more
    read-more

    Co-Processed Excipients

    read-more
    read-more

    Vegetarian Capsules

    read-more
    read-more

    API Stability Enhancers

    read-more
    read-more

    Thickeners and Stabilizers

    read-more
    read-more

    Coloring Agents

    read-more
    read-more

    Emulsifying Agents

    read-more
    read-more

    Rheology Modifiers

    read-more
    read-more

    Solubilizers

    read-more
    read-more

    Digital Content read-more

    Create Content with PharmaCompass, ask us

    DATA COMPILATION #PharmaFlow

    read-more
    read-more

    NEWS #PharmaBuzz

    read-more
    read-more

    Global Sales Information

    Do you need Business Intel? Ask us

    Market Place

    Do you need sourcing support? Ask us

    ABOUT THIS PAGE

    Ask Us for Pharmaceutical Supplier and Partner
    Ask Us, Find A Supplier / Partner
    No Commissions, No Strings Attached, Get Connected for FREE

    What are you looking for?

    How can we help you?

    The request can't be empty

    Please read our Privacy Policy carefully

    You must agree to the privacy policy

    The name can't be empty
    The company can't be empty.
    The email can't be empty Please enter a valid email.
    The mobile can't be empty

    Market Place

    Market Place

    PharmaCompass

    Home

    Market Place

    Menu

    Post Enquiry

    Post Enquiry

    Market Place

    Market Place

    Search